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Published on: November 25, 2017
A Two Birds with One Stone Strategy: Sialic Acid-Modified Pitavastatin Liposomes for Combating Atherosclerosis and
Shuang Lu1, Shuo Wang1, Xueying Tang1
1College of Pharmacy, Shenyang Pharmaceutical University, Wenhua Road, No. 103, Shenyang 110016, China.
Abstract:
Atherosclerotic cardiovascular disease (ASCVD) poses a severe threat to human health, and the global prevalence of atherosclerosis-related diseases continues to rise, necessitating urgent exploration of novel strategies. Inspired by the close links between tumors and atherosclerosis (AS), as well as the clinical reality of their comorbidity, the present study encapsulated pitavastatin within liposomes and modified them with sialic acid-cholesterol (SA-CH) to achieve targeted drug delivery via peripheral blood neutrophils (PBNs). Compared to oral pitavastatin administration, sialic acid-modified pitavastatin liposomes (PIT-SAL) demonstrated superior efficacy in attenuating disease progression in atherosclerotic mice, with sustained therapeutic effects even after treatment cessation, suggesting the potential for eradication of AS. Notably, PIT-SAL additionally exhibited antitumor potential by effectively reducing tumoral cholesterol accumulation while enhancing T-cell infiltration. Collectively, our preliminary findings highlight the great translational potential of PIT-SAL as a targeted therapy for both AS and tumors, offering a potential breakthrough in managing these interconnected diseases.
Insights
Targeted liposomes carrying pitavastatin (PIT-SAL) effectively treat atherosclerosis and tumors in mice. This novel drug delivery system shows promise for managing these interconnected diseases, even after treatment stops.
Area of Science:
- Cardiovascular Research
- Oncology
- Drug Delivery Systems
Background:
- Atherosclerotic cardiovascular disease (ASCVD) is a growing global health concern.
- Comorbidity of atherosclerosis (AS) and tumors necessitates innovative therapeutic strategies.
- Liposomes offer a platform for targeted drug delivery.
Purpose of the Study:
- To develop sialic acid-cholesterol (SA-CH) modified pitavastatin liposomes (PIT-SAL) for targeted delivery.
- To evaluate the efficacy of PIT-SAL in treating atherosclerosis and tumors.
- To investigate the therapeutic potential of PIT-SAL in managing interconnected diseases.
Main Methods:
- Encapsulation of pitavastatin into liposomes.
- Modification of liposomes with sialic acid-cholesterol (SA-CH) for targeting peripheral blood neutrophils (PBNs).
- In vivo evaluation in atherosclerotic mouse models, assessing disease progression, therapeutic effects, tumoral cholesterol, and T-cell infiltration.
Main Results:
- PIT-SAL demonstrated superior efficacy in attenuating atherosclerosis progression compared to oral pitavastatin.
- Sustained therapeutic effects of PIT-SAL were observed even after treatment cessation.
- PIT-SAL exhibited antitumor potential by reducing tumoral cholesterol and enhancing T-cell infiltration.
Conclusions:
- PIT-SAL shows significant translational potential as a targeted therapy for both atherosclerosis and tumors.
- This approach offers a promising breakthrough for managing interconnected AS and cancer.
- Targeted liposomal delivery enhances therapeutic outcomes for complex diseases.
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